Abstract: Ligands of formula (V);
bis-aryliminepyridine MXn complexes comprising a ligand of formula (V), wherein M is a metal selected from Fe and Co, n is 2 or 3, and X is halide, optionally substituted hydrocarbyl, alkoxide, amide, or hydride; [bis-aryliminepyridine MYp.Ln+] [NC31 ]q complexes, comprising a ligand of formula (V), wherein Y is a ligand which may insert an olefin, M is Fe or Co, NC− is a non-coordinating anion and p+q is 2 or 3, matching the formal oxidation of the metal atom M, L is a neutral Lewis donor molecule and n=0, 1, or 2; and processes for the production of alpha-olefins from ethylene, using said complexes.
Type:
Grant
Filed:
June 28, 2001
Date of Patent:
January 27, 2004
Assignee:
Shell Oil Company
Inventors:
Eric Johannes Maria De Boer, Harry Van Der Heijden, Nicolaas Meijboom, Arie van Zon
Abstract: &agr;-and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
May 6, 2002
Date of Patent:
January 27, 2004
Assignee:
G. D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
Abstract: Compounds of formula (I), wherein R1 and R2 are, independently of one another, H, C1-C6alkyl, C1-C6halogenalkyl, C1-C6alkoxy, C1-C6alkoxy-C1-C6alkyl, or C1-C6alkoxy-C1l-C6alkyloxy, and R3 is C1-C6alkyl, are obtainable in high yields by stereoselective addition of R3-substituted propionic acid esters to R1- and R2-substituted benzaldehydes of formula R—CHO to form corresponding 3-R-3-hydroxy-2-R3-propionic acid esters, conversion of the OH group to a leavaing group, subsequent regioselective elimination to form 3-R-2-R3-propenic acid esters, and their hydrolysis to form corresponding propenic carboxylic acids and their enantioselective hydrogenation, wherein R is (a).
Type:
Grant
Filed:
January 2, 2003
Date of Patent:
January 27, 2004
Assignee:
Speedel Pharma AG
Inventors:
Stefan Stutz, Peter Herold, Felix Spindler, Walter Weissensteiner, Thomas Sturm
Abstract: A polyether-polyol compound represented by the compositional formula C3nH6n+2O2n+1, wherein n is an integer of 4 or more, wherein the polyether-polyol compound has a total number of 1,2-diol unit and 1,3-diol unit of [(n/2)+1] in a case where n is an even number of 4 or more, or a total number of 1,2-diol unit and 1,3-diol unit of [((n−1)/2)+1] and one hydroxyl group which is not involved in the units in a case where n is an odd number of 5 or more; a polyglycerol alkyl ether, a part of hydroxyl groups in a polyglycerol being substituted by an alkyl group, wherein the polyglycerol is the polyether polyol compound mentioned above; and an ester prepared by the process comprising reacting the polyether-polyol compound mentioned above or the polyglycerol alkyl ether mentioned above with a fatty acid.
Abstract: The present invention relates to an improved method for the preparation of Artemether. Artemether prepared from the process is useful for the treatment of uncomplicated, severe complicated and multi drug resistant malaria.
Type:
Grant
Filed:
March 25, 2002
Date of Patent:
January 27, 2004
Assignee:
Council of Scientific and Industrial Research
Abstract: A process for the preparation of 1,5-dideoxy -1,5-imino hexitols of a hexose sugars from novel hydroxyl protected oxime intermediates. The process includes formation of a lactam which is reduced to the hexitol. The hexitols are useful as drugs.
Type:
Grant
Filed:
October 4, 2001
Date of Patent:
January 27, 2004
Assignee:
Board of Trustees of Michigan State University
Inventors:
Rawle I. Hollingsworth, Gabriela Pistia-Brueggeman
Abstract: Disclosed is a method for treating a disorder responsive to the positive modulation of AMPA receptors in animals suffering therefrom, comprising administering to an animal in need thereof a compound of Formula I:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
Y is NH2, NHR, and NHCOR; Z is O and S; and R1, R2, R3, R4, and X are defined herein. These compounds can be used as cognitive enhancers, for the treatment of neurodegenerative diseases, including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, AIDS associated dementia and Down's syndrome as well as for the treatment of schizophrenia and myoclonus. Also disclosed are pharmaceutical compositions useful for treating disorders responsive to the positive modulation of AMPA receptors, and novel compounds of Formula I.
Type:
Grant
Filed:
May 20, 2002
Date of Patent:
January 20, 2004
Assignee:
Euro-Celtique S.A.
Inventors:
Christopher S. Konkoy, David B. Fick, Sui Xiong Cai, Nancy C. Lan, John F. W. Keana
Abstract: Alcohol alkoxylates of the formula (I)
R1—O—(CH2—CHR5—O—)r(CH2—CH2—O—)n(CH2—CHR6—O—)s(CH2—CHR2—O—)mH (I)
where
R1 is an at least singly branched C4-22-alkyl
R2 is C3-4-alkyl
R5 is C1-4-alkyl
R6 is methyl or ethyl
n is an average value from 1 to 50
m is an average value from 0 to 20
r is an average value from 0 to 50
s is an average value from 0 to 50,
where m is at least 0.5 if R5 is methyl or ethyl or r is 0, or alcohol alkoxylates of the formula (II)
R3—O—(CH2—CH2—O—)p(CH2—CHR4—O—)qH (II)
where
R3 is branched or unbranched C4-22-alkyl
R4 is C3-4-alkyl
p is an average value of from 1 to 50
q is an average value of from 0.5 to 20
are used as low-foam or foam-suppressing surfactants.
Type:
Grant
Filed:
October 7, 2002
Date of Patent:
January 20, 2004
Assignee:
BASF Aktiengesellschaft
Inventors:
Helmut Gümbel, Martin aus dem Kahmen, Norbert Wagner, Klaus Taeger
Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
Type:
Grant
Filed:
February 15, 2002
Date of Patent:
January 20, 2004
Assignee:
ICOS Corporation
Inventors:
Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Laurence E. Burgess, Stephen T. Schlachter
Abstract: This invention relates to a 4-oxybenzopyran derivative of formula (I) wherein, R1 and R2 represent each independently a hydrogen atom, a C1-6 alkyl group or a phenyl group; R3 represents a hydroxyl group or C1-6 alkylcarbonyloxy group; R4 represents a hydrogen atom, a C3-6 cycloalkyl group, a C1-6 alkyl group, a C1-6 alkylcarbonyl group, a C1-6 alkylaminocarbonyl group, a di-C1-6 alkylaminocarbonyl group, an aryl group or a heteroaryl group; R5 represents a hydrogen atom or a C1-6 alkyl group; X is absent or represents C═O or SO2; R6 represents a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group; R7 represents a hydrogen atom, a halogen atom, a nitro group or a cyano group; or a pharmaceutically acceptable salt thereof. And this invention also relates to a drug for treating arrhytmia having the prolongation effect on the functional refractory period comprising said compound or a pharmaceutically acceptable salt thereof as an active ingredient.
Abstract: The invention pertains to a novel composition comprising guaifenesin tannate and to a method for preparing guaifenesin tannate by reacting guaifenesin with tannic acid at a temperature above the melting point of guaifenesin. The guaifenesin tannate has extended release properties and is useful in pharmaceutical compositions as an expectorant in warm-blooded animals or as a muscle relaxant in non-human animals.
Abstract: Compounds of the formula (I) and also process for preparing them
where substituents X1, X2, Y and Z are defined as follows:
X1 is H or F
X2 is H or F
Y is CI, Br, or I
Z is CHO or COOH or CN
n is 0 or 1
and also their use as starting material for preparing agrochemicals, electronics materials and pharmaceuticals.
Abstract: This invention encompasses the Form V polymorph of Compound A of structural formula:
which is useful in the treatment of cyclooxygenase-2 mediated diseases. The invention encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising the Form V polymorph of Compound A. The invention also encompasses a process for synthesizing the Form V polymorph of Compound A.
Type:
Grant
Filed:
January 14, 2003
Date of Patent:
January 6, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Louis S. Crocker, Ian W. Davies, Richard G. Osifchin, Andrew Kotliar
Abstract: A process for working up distillation residues from the synthesis of tolylene diisocyanate by reaction of the distillation residues with water comprises reacting the TDI distillation residues with water in a continuous or semicontinuous process in a backmixed reactor in the presence of hydrolysate.
Type:
Grant
Filed:
December 14, 2000
Date of Patent:
January 6, 2004
Assignee:
BASF Aktiengesellschaft
Inventors:
Hans Volkmar Schwarz, Markus Maurer, Michael Sander, Eckhard Ströfer, Rene Leuthold, Burghard Hantel, Siegfried Richter, Jörg Therre
Abstract: The present invention relates to processes for the preparation of a compound of the formula
wherein W is nitrogen or —CR3; R1 is halogen, haloalkyl, haloalkoxy, R4S(O)n— or —SF5; R2 is hydrogen; R3 is halogen; R4 is alkyl or haloalkyl; and n is 0, 1 or 2.
Abstract: A compound of formula (I)
wherein:
R isopropyl;
n is 0;
R1 is naphthylmethyl;
R2 is t-butyl; and
R3 is methyl;
is useful in the treatment of disorders mediated by s-CD23.
Abstract: A method for producing alkoxy malonic acid dinitrites of general formula (I),
wherein R1 means C1-6-alkyl or halogen-substituted C1-6-alkyl. The method involves converting the corresponding alkoxy malonic acid diamides of general formula (II),
wherein R1 has the aforementioned meaning, by means of a dehydrating agent. The intermediate products of general formula (III),
whereby the products are formed during dehydration.
Type:
Grant
Filed:
October 11, 2002
Date of Patent:
January 6, 2004
Assignee:
Lonza AG
Inventors:
Johannes Bartek, Rudolf Fuchs, Stefan Hildbrand
Abstract: A method of increasing the fluorous nature of a compound includes the step of reacting the compound with at least one second compound having the formula:
wherein Rf is a fluorous group and m is 0, 1 or 2.
Abstract: The present invention provides processes for purifying 6-methoxy omeprazole, products using such processes, pharmaceutical formulations using such products, and methods of using such products for gastric acid inhibition.
Type:
Grant
Filed:
April 20, 2001
Date of Patent:
January 6, 2004
Inventors:
Linda B. Whittall, Grayson Walker Stowell, Robert R. Whittle
Abstract: Disclosed herein is a process for preparing a reaction product containing methylene diphenylamine, comprising reacting aniline and formaldehyde in the presence of an acid catalyst wherein the acid level of the resulting reaction mixture is reduced during digestion of the reaction mixture.
Type:
Grant
Filed:
December 29, 1999
Date of Patent:
January 6, 2004
Assignee:
Bayer Polymers LLC
Inventors:
Louis Renbaum, Mark S. Solomon, William D. Tippins